IP Library Granted Patent US 9,499,511
Granted Patent B2
US 9,499,511 · App. 14/927,039 · Granted Nov 22, 2016

N-substituted hydroxylamine derivatives with carbon-based leaving groups

Inventors: John P. Toscano (Glen Arm, MD); Daryl A. Guthrie (Baltimore, MD)
Assignee: The Johns Hopkins University
C07D319/06C07D231/08C07D231/22C07D231/46C07D239/62
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,499,511
App. No.
14/927,039
Granted
Nov 22, 2016
Kind
B2
Abstract

The disclosed subject matter provides certain N-substituted hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or development of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.

Claims (28)

1. A compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein:

X and Z —NR 3 ;

Y is selected from —C(═O)—, —C(═S)—, —C(═NR 5 )—, and —CR 5 R 6 —;

R is selected from C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, C 1 -C 8 alkoxy, C 5 -C 10 aryl, —C(═O)R 7 , —C(═S)R 7 , —C(═NR 7 )R 8 , and —C(═NOR 7 )R 8 , wherein the alkyl, alkenyl, alkynyl, alkoxy and aryl are unsubstituted or substituted with one or more substituents; and

R 3 , R 5 , R 6 , R 7 and R 8 are independently selected from —H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, C 5 -C 10 aryl, C 5 -C 10 heterocycloalkyl, C 5 -C 10 heterocycloalkenyl, and C 5 -C 10 heteroaryl wherein the alkyl, alkenyl, alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl and heteroaryl are unsubstituted or substituted with one or more substituents.

2. The compound of claim 1 , wherein R is C 1 -C 8 alkyl, wherein the alkyl is unsubstituted or substituted with one or more substituents.

3. The compound of claim 1 , wherein R is C 1 -C 4 alkyl.

4. The compound of claim 1 , wherein R is —C(═NOR 5 )R 6 .

5. The compound of claim 1 , wherein R is —C(═NOR 5 )R 6 ; and R 5 and R 6 are independently C 1 -C 4 alkyl.

6. The compound of any one of claims 1 , and 2 to 5 , wherein X and Z are each —NR 3 —; and R 3 is C 1 -C 4 alkyl.

7. The compound of any one of claims 1 , and 2 to 5 , wherein Y is —CR 5 R 6 —.

8. The compound of any one of claims 1 , and 2 to 5 , wherein Y is —C(═O)—.

9. The compound of claim 1 , wherein the compound is:

10. A pharmaceutical composition comprising:

a compound of claim 1 ; and

a pharmaceutically acceptable excipient.

11. A method of treating a disease or condition selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy, comprising administering a compound of claim 1 to a subject in need thereof.

12. A method of modulating in vivo nitroxyl levels, comprising administering a compound of claim 1 to a subject in need thereof.

13. A kit comprising:

a compound of claim 1 ; and

instructions for treating a condition that is responsive to nitroxyl therapy.

14. The compound of any one of claims 1 and 2 to 5 , wherein X and Z are each

—NR 3 —; and Y is —CR 5 R 6 —.

15. The compound of any one of claims 1 and 2 to 5 , wherein X and Z are each

—NR 3 —; R 3 is C 1 -C 4 alkyl; and Y is —CR 5 R 6 —.

16. The compound of any one of claims 1 and 2 to 5 , wherein X and Z are each —NR 3 —; and Y is —C(═O)—.

17. The compound of any one of claims 1 and 2 to 5 , wherein X and Z are each —NR 3 —; R 3 is C 1 -C 4 alkyl; and Y is —C(═O)—.

Assignments (2)
CONFIRMATORY LICENSE Recorded Dec 28, 2017
From: JOHNS HOPKINS UNIVERSITY
To: NATIONAL SCIENCE FOUNDATION
Reel/Frame 044969/0088 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 30, 2015
From: TOSCANO, JOHN P.; GUTHRIE, DARYL A.
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 036926/0934 →
Continuity (3)
Division 14352399
Provisional Application 61548036 · Oct 17, 2011
Related Publication 20160115148A1 · Apr 28, 2016